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Tobramycin liposome used for aerosol inhalation and production method thereof

A technology of tobramycin lipid and atomized inhalation, which is applied in liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of low bioavailability, thermal instability, Difficulty crossing cell membranes, etc.

Active Publication Date: 2020-06-05
ZHUHAI ESSEX BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] In order to bring into play the advantages of tobramycin in the treatment of patients with ventilator-associated pneumonia and cystic fibrosis, and overcome the problems of low bioavailability of traditional injection and oral administration, the inhalation of tobramycin will produce Phlegm antagonism, that is, the mucin in the sputum is combined with the drug to affect its antibacterial activity. In addition, tobramycin has high water solubility, is difficult to pass through the cell membrane, and has disadvantages such as thermal instability. The purpose of the present invention is to prepare a drug with stable physical and chemical properties. A new dosage form of tobramycin

Method used

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  • Tobramycin liposome used for aerosol inhalation and production method thereof
  • Tobramycin liposome used for aerosol inhalation and production method thereof
  • Tobramycin liposome used for aerosol inhalation and production method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0088] A kind of tobramycin liposome for nebulization inhalation, it comprises the following components according to the total mass percentage of raw materials:

[0089]

[0090]

[0091] Preparation:

[0092] 1) Precisely weigh the protein lecithin, cholesterol and vitamin E in the prescribed amount, dissolve them in absolute ethanol (accounting for 25% of the total amount), dissolve in a water bath at 55°C, and form an organic phase solution;

[0093] 2) Accurately weigh the prescription amount of tobramycin and chitosan dissolved in pH7.0 phosphate buffer (accounting for 75% of the total amount) as the water phase;

[0094] 3) Using a syringe, slowly add the organic phase to the aqueous phase with constant temperature magnetic stirring at 55°C, and stir for 30 minutes;

[0095] 4) Evaporate under reduced pressure to remove the organic solvent, and then filter through a 0.45 μm microporous membrane to obtain tobramycin liposomes. Its drawing is attached figure 1 sho...

Embodiment 2

[0097] A kind of tobramycin liposome for nebulization inhalation, it comprises the following components according to the total mass percentage of raw materials:

[0098]

[0099] Preparation:

[0100] 1) Accurately weigh the egg yolk lecithin, cholesterol and vitamin E of the prescribed amount, dissolve them in an appropriate amount of ethanol (25%), dissolve them completely by ultrasonic, and use them as the organic phase.

[0101] 2) Precisely weigh the prescribed amount of tobramycin and dissolve it in pH 7.0 phosphate buffer as the water phase.

[0102] 3) The water phase was injected into the organic phase, and the water bath was sonicated for 4 minutes to prepare a stable emulsion.

[0103] 4) Transfer to a round-bottomed flask again, in a water bath at 50°C for 100r·min -1 , evaporated under reduced pressure to remove the organic solvent to a viscous gummy solution. Then add an appropriate amount of aqueous medium for elution. After the elution is complete, use a ...

Embodiment 3

[0105] A kind of tobramycin liposome for nebulization inhalation, it comprises the following components according to the total mass percentage of raw materials:

[0106]

[0107] Preparation:

[0108] 1) Precisely weigh the egg yolk lecithin, cholesterol and vitamin E in the prescribed amount, place them in a round bottom flask, and add an appropriate amount of ethanol (25%) for ultrasonic dissolution.

[0109] 2) Put it on a rotary evaporator again, put it in a water bath at 50°C for 100 r·min-1, and remove the organic solvent by rotary evaporation under reduced pressure, so that the lipid forms a thin film on the bottle wall.

[0110] 3) Weigh the prescribed amount of tobramycin and dissolve it in phosphate buffer solution of pH 7.0, then add it into the round bottom flask, continue to rotate and hydrate completely, and obtain a milky white suspension, ultrasonicate for 5 minutes with a 100W probe (working 3s , intermittent 3s), after using a 0.45 μm microporous membrane...

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Abstract

The invention discloses a tobramycin liposome used for aerosol inhalation. The tobramycin liposome used for aerosol inhalation is composed of the following components: 0.1%-15.0% of tobramycin, 0.5%-36.0% of a phospholipid, 0.05%-20.0% of a stabilizer, 0.01%-10.0% of a charge modifier, 0.01%-5.0% of an antioxidant, 5.0%-50.0% of an organic-phase medium and the balance an aqueous-phase medium. According to the tobramycin liposome used for aerosol inhalation, the aerosol inhalation technology is used, relative to oral administration, the aerosol inhalation technology has the advantages that a medicine can be directly delivered to a respiratory tract, is absorbed fast, and takes effect quickly, and a medicine concentration of the respiratory tract is increased; the bioavailability and the stability are high, and the tobramycin liposome used for aerosol inhalation has good safety; and a production process is simple, easy and reasonable, and the performance is stable, so that conditions arecreated for achieving industrial productization.

Description

technical field [0001] The present invention relates to the technical field of pharmaceutical preparations, specifically a kind of tobramycin liposome for nebulization inhalation and a preparation method thereof. Background technique [0002] Tobramycin is an aminoglycoside antibiotic naturally produced by Streptomyces, which mainly causes changes in the permeability of the cell membrane, progressive destruction of the outer membrane of the cell, and final cell death by inhibiting protein synthesis. Bactericidal at inhibitory concentrations. It is an aminoglycoside antibiotic with less clinical drug resistance. It has good antibacterial activity against most Enterobacteriaceae bacteria and Staphylococcus. Pseudomonas aeruginosa, Haemophilus, Staphylococcus aureus, Klein pneumoniae in adults and children over 6 years old (including 6 years old) with bronchiectasis, ventilator-associated pneumonia (VAP) and cystic fibrosis It is used as the first-line treatment drug for earl...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/702A61K47/24A61K47/28A61K47/36A61K47/22A61K47/10A61P31/04
CPCA61K9/127A61K9/0078A61K31/702A61K47/24A61K47/28A61K47/36A61K47/22A61K47/10A61P31/04
Inventor 张树荣严贤龙薛琦田霞牛璐王振恒
Owner ZHUHAI ESSEX BIO PHARMA
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